PT1648922E - Compostos macrocíclicos espacialmente definidos úteis para descoberta de fármacos - Google Patents

Compostos macrocíclicos espacialmente definidos úteis para descoberta de fármacos Download PDF

Info

Publication number
PT1648922E
PT1648922E PT04761605T PT04761605T PT1648922E PT 1648922 E PT1648922 E PT 1648922E PT 04761605 T PT04761605 T PT 04761605T PT 04761605 T PT04761605 T PT 04761605T PT 1648922 E PT1648922 E PT 1648922E
Authority
PT
Portugal
Prior art keywords
compound
λλγ
quot
figura
formula
Prior art date
Application number
PT04761605T
Other languages
English (en)
Portuguese (pt)
Inventor
Pierre Deslongchamps
Yves Dory
Mark Peterson
Kamel Benakli
Eric Marsault
Luc Ouellet
Mahesh Ramaseshan
Martin Vezina
Daniel Fortin
Ruoxi Lan
Shigui Li
Gerald Villeneuve
Hamid Hoveyda
Sylvie Beaubien
Graeme Fraser
Original Assignee
Tranzyme Pharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tranzyme Pharma Inc filed Critical Tranzyme Pharma Inc
Publication of PT1648922E publication Critical patent/PT1648922E/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
PT04761605T 2003-07-31 2004-08-02 Compostos macrocíclicos espacialmente definidos úteis para descoberta de fármacos PT1648922E (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US49124803P 2003-07-31 2003-07-31

Publications (1)

Publication Number Publication Date
PT1648922E true PT1648922E (pt) 2011-01-04

Family

ID=34115484

Family Applications (1)

Application Number Title Priority Date Filing Date
PT04761605T PT1648922E (pt) 2003-07-31 2004-08-02 Compostos macrocíclicos espacialmente definidos úteis para descoberta de fármacos

Country Status (15)

Country Link
US (3) US7452862B2 (de)
EP (3) EP2316846B1 (de)
JP (1) JP4928262B2 (de)
AT (1) ATE490264T1 (de)
AU (1) AU2004261329B2 (de)
CA (1) CA2533818C (de)
CY (1) CY1111901T1 (de)
DE (1) DE602004030344D1 (de)
DK (1) DK1648922T3 (de)
ES (1) ES2357235T7 (de)
IL (1) IL173312A0 (de)
PL (1) PL1648922T3 (de)
PT (1) PT1648922E (de)
SI (1) SI1648922T1 (de)
WO (1) WO2005012331A1 (de)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004111077A1 (en) * 2003-06-18 2004-12-23 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
USRE42624E1 (en) 2003-06-18 2011-08-16 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
USRE42013E1 (en) 2003-06-18 2010-12-28 Tranzyme Pharma Inc. Macrocyclic modulators of the ghrelin receptor
US7491695B2 (en) * 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
US8921521B2 (en) 2003-06-18 2014-12-30 Ocera Therapeutics, Inc. Macrocyclic modulators of the Ghrelin receptor
EP1648923B1 (de) * 2003-07-31 2008-12-31 Tranzyme Pharma Inc. Räumlich definierte makrocyclen, die peptidbindungssurrogate enthalten
JP5739766B2 (ja) * 2004-06-18 2015-06-24 オセラ セラピューティクス, インコーポレイテッド グレリン受容体の大環状モジュレーターの使用方法
WO2006046977A1 (en) * 2004-10-26 2006-05-04 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and methods of using the same
CA2583345A1 (en) * 2005-06-13 2006-12-28 Tranzyme Pharma, Inc. Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same
MY150098A (en) * 2005-07-26 2013-11-29 Glaxo Group Ltd Benzylpiperazine derivates and their medical use
US8088733B2 (en) * 2006-07-06 2012-01-03 Tranzyme Pharma Inc. Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders
JP5684474B2 (ja) * 2006-09-11 2015-03-11 オセラ セラピューティクス, インコーポレイテッド 胃腸の運動障害疾患の治療のためのモチリン受容体の大環状アンタゴニスト
EP2118080B1 (de) * 2007-02-09 2016-08-31 Ocera Therapeutics, Inc. Makrocyclische ghrelin-rezeptormodulatoren und verwendungsverfahren dafür
US20080287371A1 (en) * 2007-05-17 2008-11-20 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor for modulation of the migrating motor complex
WO2010047982A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CA2741672A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
KR101575703B1 (ko) 2009-02-27 2015-12-10 라퀄리아 파마 인코포레이티드 모틸린 수용체에 대해 작용제 활성을 가진 옥시인돌 유도체
US9662126B2 (en) 2009-04-17 2017-05-30 Arthrosurface Incorporated Glenoid resurfacing system and method
JP2013509434A (ja) 2009-10-30 2013-03-14 トランザイム・ファーマ,インコーポレイテッド 大環状グレリン受容体アンタゴニストおよびインバースアゴニストならびにその使用方法
WO2011106273A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2011105310A1 (en) * 2010-02-26 2011-09-01 Semiconductor Energy Laboratory Co., Ltd. Semiconductor device
EP2659404B1 (de) 2010-12-29 2018-08-08 Sigma-Aldrich Co., LLC Zellen mit gestörter expression von in adme und toxikologieverfahren involvierten proteinen
EA025380B1 (ru) 2011-02-25 2016-12-30 Мерк Шарп Энд Домэ Корп. Новые циклические производные азабензимидазола, используемые в качестве антидиабетических агентов
KR20150036245A (ko) 2012-08-02 2015-04-07 머크 샤프 앤드 돔 코포레이션 항당뇨병 트리시클릭 화합물
CN103113404B (zh) * 2013-02-22 2015-09-23 广州巨元生化有限公司 一种制备4-二烃氧基膦酰基-2-甲基-2-丁烯酸烃基酯的方法
RU2015140066A (ru) 2013-02-22 2017-03-30 Мерк Шарп И Доум Корп. Противодиабетические бициклические соединения
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US9119832B2 (en) 2014-02-05 2015-09-01 The Regents Of The University Of California Methods of treating mild brain injury
WO2017049383A1 (en) 2015-09-24 2017-03-30 Cyclenium Pharma Inc. Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same
MX2018005236A (es) 2015-10-27 2018-08-15 Hoffmann La Roche Macrociclos peptidicos contra acinetobacter baumannii.
WO2017075535A1 (en) 2015-10-28 2017-05-04 Oxeia Biopharmaceuticals, Inc. Methods of treating neurodegenerative conditions
EP3458630A4 (de) * 2016-05-16 2020-01-08 Cyclenium Pharma Inc. Bibliotheken aus verschiedenen makrocyclischen verbindungen und verfahren zur herstellung und verwendung davon
US20180110824A1 (en) * 2016-10-21 2018-04-26 Ocera Therapeutics, Inc. Macrocyclic Modulators of the Ghrelin Receptor
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
US10968232B2 (en) 2016-12-20 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
EP3388444A1 (de) * 2017-04-10 2018-10-17 F. Hoffmann-La Roche AG Antibakterielle peptidmakrozyklen und verwendung davon
WO2018232062A1 (en) 2017-06-15 2018-12-20 University Of Washington Macrocyclic polypeptides
US11505573B2 (en) 2018-03-28 2022-11-22 Hoffmann-La Roche Inc. Peptide macrocycles against Acinetobacter baumannii
US11819532B2 (en) 2018-04-23 2023-11-21 Hoffmann-La Roche Inc. Peptide macrocycles against Acinetobacter baumannii
SG11202108026UA (en) * 2019-02-08 2021-08-30 Socpra Sciences Sante Et Humaines S E C Neurotensinergic agonists and methods of using same preventing or treating pain

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2235377A1 (de) * 1971-07-30 1973-02-08 Banyu Pharma Co Ltd 2,4-thiazol-dimethanol-carbamat und verfahren zu dessen herstellung
GB1365201A (en) 1971-07-30 1974-08-29 Banyu Pharma Co Ltd 2 4 thiazoledimethanol carbamates and 2 4-thiazoledimethanol
US3997540A (en) * 1975-07-21 1976-12-14 Burroughs Wellcome Co. O [(O-piperazinocarbonyl-phenyl)-thio]-benzoates
US4382090A (en) * 1980-10-02 1983-05-03 Eli Lilly And Company N-Thiazolylmethylthioalkyl-N'alkylamidines and related compounds
US5514786A (en) * 1990-01-11 1996-05-07 Isis Pharmaceuticals, Inc. Compositions for inhibiting RNA activity
JPH10512570A (ja) 1995-01-20 1998-12-02 モレキュメティックス リミテッド コンホメーション的に制限された逆ターンライブラリおよびそれらに関連する方法
US5646285A (en) 1995-06-07 1997-07-08 Zymogenetics, Inc. Combinatorial non-peptide libraries
US5891737A (en) 1995-06-07 1999-04-06 Zymogenetics, Inc. Combinatorial non-peptide libraries
IL117426A (en) * 1996-03-10 2005-09-25 Yissum Res Dev Co Synthetic pseudopeptides having osteogenic activity and pharmaceutical compositions containing the same
US5712253A (en) 1996-06-18 1998-01-27 Abbott Laboratories Macrocyclic 13-membered ring derivatives of erythromycins A and B
US6011155A (en) * 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
EP1015479A4 (de) 1997-04-11 2002-07-24 Lilly Co Eli Kombinatorische substanzbibliotheken von peptidomimetischen makrocyclen sowie die dazugehörigen verfahren
US20020068301A1 (en) 1997-05-28 2002-06-06 Hung-Sen Lai Cyclic peptide libraries and methods of use thereof to identify binding motifs
US6165985A (en) * 1998-02-13 2000-12-26 Solvay Pharmaceuticals Gmbh 11-acetyl-12,13-dioxabicyclo[8.2.1]-tridecenone derivatives, processes for their preparation and pharmaceutical compositions comprising them
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
ATE446758T1 (de) * 2000-05-31 2009-11-15 Pfizer Prod Inc Verwendung von wachstumshormonsekretagoga zur förderung der beweglichkeit des verdauungstrakts
AU2001283938A1 (en) 2000-07-24 2002-02-05 Ardana Bioscience Limited Ghrelin antagonists
US6653334B1 (en) 2002-12-27 2003-11-25 Kowa Co., Ltd. Benzoxazole compound and pharmaceutical composition containing the same
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
US7491695B2 (en) * 2003-06-18 2009-02-17 Tranzyme Pharma Inc. Methods of using macrocyclic modulators of the ghrelin receptor
WO2004111077A1 (en) * 2003-06-18 2004-12-23 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor
EP1648923B1 (de) * 2003-07-31 2008-12-31 Tranzyme Pharma Inc. Räumlich definierte makrocyclen, die peptidbindungssurrogate enthalten
MXPA06002435A (es) 2003-09-03 2006-06-20 Kowa Co Compuesto activador del receptor activado por el proliferador de peroxisoma y composicion farmaceutica que lo contiene.

Also Published As

Publication number Publication date
EP1648922B3 (de) 2012-08-15
EP1648922A4 (de) 2006-08-23
JP4928262B2 (ja) 2012-05-09
ES2357235T3 (es) 2011-04-20
CY1111901T1 (el) 2015-11-04
EP2316846B1 (de) 2019-10-02
DK1648922T3 (da) 2011-03-14
US8440851B2 (en) 2013-05-14
DE602004030344D1 (de) 2011-01-13
EP2319859B1 (de) 2013-03-27
AU2004261329B2 (en) 2011-10-27
PL1648922T3 (pl) 2011-05-31
ES2357235T7 (es) 2013-02-14
CA2533818C (en) 2015-03-17
EP2316846A2 (de) 2011-05-04
IL173312A0 (en) 2009-02-11
AU2004261329A1 (en) 2005-02-10
SI1648922T1 (sl) 2011-03-31
WO2005012331A1 (en) 2005-02-10
EP1648922A1 (de) 2006-04-26
US20090137817A1 (en) 2009-05-28
ES2357235T8 (es) 2011-06-06
EP2316846A3 (de) 2012-04-04
EP2319859A2 (de) 2011-05-11
EP1648922B9 (de) 2013-04-03
ATE490264T1 (de) 2010-12-15
US20050137127A1 (en) 2005-06-23
EP2319859A3 (de) 2011-12-21
US20110237785A1 (en) 2011-09-29
CA2533818A1 (en) 2005-02-10
EP1648922B1 (de) 2010-12-01
US8022252B2 (en) 2011-09-20
US7452862B2 (en) 2008-11-18
JP2007527863A (ja) 2007-10-04

Similar Documents

Publication Publication Date Title
PT1648922E (pt) Compostos macrocíclicos espacialmente definidos úteis para descoberta de fármacos
RU2756273C2 (ru) Полиморфные модификации n-[(3-фтор-4-метоксипиридин-2-ил)метил]-3-(метоксиметил)-1-({ 4-[(2-оксопиридин-1-ил)метил]фенил} метил)пиразол-4-карбоксамида и их соли
ES2226482T3 (es) Inhibidores de trombina.
ES2309537T3 (es) Derivados de amida heterociclica que poseen actividad inhibidora de la glucogeno fosforilasa.
ES2627633T3 (es) Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]piracin-3(2H)-ona como inhibidores de beta-secretasa (BACE)
CA2635580A1 (en) Substituted bis-amide metalloprotease inhibitors
BRPI0712021A2 (pt) composto e composiÇÕes como inibidores da protease ativadora de canal
ES2315676T3 (es) Derivados de indolamida que poseen actividad inhibidora de la glucogeno fosforilasa.
KR20040091101A (ko) 글리코겐 포스포릴라제 억제 활성을 갖는 헤테로시클릭아미드 유도체
CN104284891A (zh) 构象受限的全合成大环化合物
JP2019527672A (ja) 多様な大環状化合物のライブラリならびにその製造方法および使用方法
CA2477717A1 (en) Indolamid derivatives which possess glycogen phosphorylase inhibitory activity
Bag et al. Synthesis, photophysical properties of triazolyl-donor/acceptor chromophores decorated unnatural amino acids: Incorporation of a pair into Leu-enkephalin peptide and application of triazolylperylene amino acid in sensing BSA
CA2998885A1 (en) Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same
Zhao et al. Synthesis of new class dipeptide analogues with improved permeability and antithrombotic activity
CA3152264A1 (en) Pyrazole compounds, formulations thereof, and a method for using the compounds and/or formulations
Reddy et al. Synthesis of small cyclic peptides via intramolecular Heck reactions
Wei et al. Discovery of new Lenalidomide derivatives as potent and selective GSPT1 degraders
EP1845104A1 (de) Par-ii-agonist
US20150239890A1 (en) Crystal of n-[2-(amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide
Friedrichsen et al. Application of enzymatically stable dipeptides for enhancement of intestinal permeability. Synthesis and in vitro evaluation of dipeptide-coupled compounds
CN103781915A (zh) 氯氮平免疫测定方法
US20060199966A1 (en) Indol-2-amides as glycogen phosphorylase inhibitors
JP2004537594A (ja) ジスルフィドリガンドおよびチオスルホネートリガンド、ならびにこれらのリガンドを含むライブラリー
EP1864994B1 (de) Par-2-agonist